Molecule Details
InChIKeyHLWURFKMDLAKOD-UHFFFAOYSA-N
Compound NameGefapixant
Canonical SMILESCOc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)2
Pfam Stratification Homologous
Avg pChEMBL7.0
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB15097
Drug NameGefapixant
CAS Number1015787-98-0
Groups approved investigational
ATC Codes R05DB29 G01AE10
DescriptionIt has been estimated that 5-10% of adults globally suffer from chronic cough, which is defined as a cough lasting longer than eight weeks.[L48601] A subset of these patients remain symptomatic despite thorough investigation and treatment, termed refractory chronic cough (RCC) if they have a cough t...

Categories: Amides BCRP/ABCG2 Substrates Benzene Derivatives Cough and Cold Preparations MATE 1 Substrates MATE 2 Substrates MATE substrates P-glycoprotein substrates Sulfonamides Sulfones Sulfur Compounds
Cross-references: BindingDB: 50533006 CHEMBL3716057 ChemSpider: 58828660 PDB: AF9 Wikipedia: Gefapixant ZINC: ZINC000116342482
Target Activities (2)
Target Gene Organism Category Pfam pChEMBL Type Source
P56373 P2RX3 Homo sapiens Human PF00864 7.3 IC50 ChEMBL;BindingDB
Q9UBL9 P2RX2 Homo sapiens Human PF00864 6.7 IC50 ChEMBL
DrugBank Target Actions (7)
Target Gene Target Name Action Type
P56373 P2RX3 P2X purinoceptor 3 antagonist targets
Q9UBL9 P2RX2 P2X purinoceptor 2 antagonist targets
P56373 P2RX3 P2X purinoceptor 3 inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters
Q86VL8 SLC47A2 Multidrug and toxin extrusion protein 2 substrate transporters
Q96FL8 SLC47A1 Multidrug and toxin extrusion protein 1 substrate transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 substrate transporters